Highly efficient synthesis of DNA binding polyamides for commercial exploitation

基因转录是发生在每个活细胞中的一个中心生物学过程。它包括读取存储在细胞DNA中的遗传信息，并将其转化为RNA。人工调控这一过程的能力是生物技术和医学中一个备受追捧的目标，因为它将提供一种工具，可以验证新的药物靶点，研究新的生物学，以及提供新的治疗方法。DNA结合聚酰胺是一种能够调节基因转录的小分子。它们是唯一一类几乎可以针对任何DNA序列的小分子，但广泛采用的一个重大障碍是能够以快速、经济有效的方式高产率和高纯度地制造各种聚酰胺。莱斯特开发了一种合成DNA结合聚酰胺的新方法，使其能够以高产率、高纯度和低成本制备，从而克服了进入市场的主要障碍。与ART的当前状态相比，莱斯特方法的总体产量提高了330倍。这个后续基金项目的目的是自动化和优化可扩展的聚酰胺生产，并进一步由最终用户和许可证持有人进行生物验证。这些商业化前的活动将加强专利技术的商业化，并为其在生物和医学中的广泛应用奠定基础。

Gene transcription is a central biological process that occurs in every living cell. It involves reading the genetic information stored in the cell's DNA and converting this into RNA. The ability to artificially regulate this process is a highly sought after goal in biotechnology and medicine as it would offer a tool that could validate new drug targets, investigate new biology as well as providing new therapeutics. DNA binding polyamides are small molecules that can regulate gene transcription. They are the only class of small molecules that can target virtually any DNA sequence, yet a significant barrier to widespread adoption is the ability to manufacture diverse collections of polyamides in high yield and purity in a quick cost-effective manner. A novel method for the synthesis of DNA-binding polyamides has been developed at Leicester that enables their preparation in high yield and purity and at low cost; thus overcoming the major barrier to market entry. The Leicester method results in increases in overall yield of up to 330-fold relative to the current state of the art.The aim of this Follow-on Fund project is to automate and optimise the scalable production of polyamides and to further biological validation by end users and licensees. These pre-commercialisation activities will enhance the patented technology for commercialisation and lay the foundation for their widespread utilisation in biology and medicine.